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Immunosuppressant
Immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK506 binding protein and to inhibit the Ca2+-dependent phosphatase and protein phosphatase 2B (PP2B; calcineurin). Activates NF-κB through phosphorylation and degradation of IκBα.
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Product Details
| Alternative Name |
Tacrolimus |
|---|---|
| Appearance |
White to off-white crystalline powder. |
| CAS |
104987-11-3 |
| Couple Target |
FKBP, Serine/threonine-protein phosphatase |
| Couple Type |
Inhibitor, Ligand |
| Formula |
C44H69NO12 |
| Identity |
FT-IR |
| MI |
14: 9025 |
| MW |
804.0 |
| Purity |
≥98% (HPLC) |
| RTECS |
KD4200000 |
| Solubility |
Soluble in DMSO, 100% ethanol, methanol, ethyl acetate or acetone; insoluble in water. |
| Source |
Isolated from Streptomyces tsukubaensi. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Handling |
Protect from light. |
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Zebrafish Larvae Position Tracker (Z-LaP Tracker): a high-throughput deep-learning behavioral approach for the identification of calcineurin pathway-modulating drugs using zebrafish larvae: S.V. Gore, et al.; Sci. Rep. 13, 3174 (2023), Abstract
- Specification of skeletal muscle fiber-type is determined by the calcineurin/NFATc1 signaling pathway during muscle regeneration: J. Shin, et al.; Biochem. Biophys. Res. Commun. 659, 20 (2023), Abstract
- Dynamic changes in β-cell [Ca 2+] regulate NFAT activation, gene transcription, and islet gap junction communication: J.G. Miranda, et al.; Mol. Metab. 57, 101430 (2022), Abstract
- Novel use of FDA-approved drugs identified by cluster analysis of behavioral profiles: S.T. Edmister, et al.; Sci. Rep. 12, 6120 (2022), Abstract
- Fluorescence imaging detection of nanodomain redox signaling events at organellar contacts: D.M. Booth, et al.; STAR Protoc. 3, 101119 (2022), Abstract — Full Text
- Calcineurin/NFATc2 and PI3K/AKT signaling maintains β-cell identity and function during metabolic and inflammatory stress: Darden, C. M., Vasu, S., et al.; iScience 25, 104125 (2022), Abstract
- Oxidative bursts of single mitochondria mediate retrograde signaling toward the ER: D.M. Booth, et al.; Mol. Cell 81, 3866 (2021), Abstract — Full Text
- Safety and efficacy of tacrolimus-coated silicone plates as an alternative to mitomycin C in a rabbit model of conjunctival fibrosis: S.Y. Yoon, et al.; PLoS One 14, e0219194 (2019), Abstract — Full Text
- Calcineurin A beta deficiency ameliorates HFD-induced hypothalamic astrocytosis in mice: K. Pfuhlmann, et al.; J. Neuroinflammation 15, 35 (2018), Abstract — Full Text
- Subcellular Distribution of HDAC1 in Neurotoxic Conditions Is Dependent on Serine Phosphorylation: Zhu, Y., Vidaurre, O. G., et al.; J. Neurosci. 37, 7547 (2017), Abstract
- Perturbed Calcineurin-NFAT Signaling Is Associated with the Development of Alzheimer’s Disease: M. Asai, et al.; Biol. Pharm. Bull. 39, 1646 (2016), Application(s):, Abstract — Full Text
- The Sur1-Trpm4 channel regulates NOS2 transcription in TLR4-activated microglia: D.B. Kurland, et al.; J. Neuroinflammation 13, 130 (2016), Application(s): Cell culture, Abstract — Full Text
- Tacrolimus Modulates TGF-β Signaling to Induce Epithelial-Mesenchymal Transition in Human Renal Proximal Tubule Epithelial Cells: J. Bennett, et al.; J. Clin. Med. 5, 50 (2016), Application(s): Cell treatment, Abstract
- Effects of embryonic cyclosporine exposures on brain development and behavior: D.E. Clift, et al.; Behav. Brain Res. 282, 117 (2015), Application(s): Cell Culture, Abstract
- Mitotic phosphatase activity is required for MCC maintenance during the spindle checkpoint: Foss, K. M., Robeson, A. C., et al.; Cell Cycle 15, 225 (2015), Abstract
- Distinct biological activity of threonine monophosphorylated MAPK isoforms during the stress response in fission yeast: B. Vazquez, et al.; Cell. Signal. 27, 2534 (2015), Application(s): Cell Culture, Abstract
- Feedback Mechanisms Regulate Ets variant 2 (Etv2) Gene Expression and Hematoendothelial Lineages: N. Koyano-Nakagawa, et al.; J. Biol. Chem. 290, 28107 (2015), Application(s): Calcineurin inhibition, Abstract — Full Text
- IRAK4 turns IL-10+ phospho-FOXO+ monocytes into pro-inflammatory cells by suppression of protein kinase B: Over, B., Ziegler, S., et al.; Eur. J. Immunol. 43, 1630 (2013), Abstract
- Phosphorylation of huntingtin at Ser421 in YAC128 neurons is associated with protection of YAC128 neurons from NMDA-mediated excitotoxicity and is modulated by PP1 and PP2A: Metzler, M., Gan, L., et al.; J. Neurosci. 30, 14318 (2010), Abstract
- A rapid HPLC-MS/MS method for the simultaneous quantification of cyclosporine A, tacrolimus, sirolimus and everolimus in human blood samples: Seger, C., Tentschert, K., et al.; Nat. Protoc. 4, 526 (2009), Abstract
- A review of the action of tacrolimus (FK506) on experimental models of rheumatoid arthritis: S. Miyata, et al.; Inflamm. Res. 54, 1 (2005), Review, Abstract
- FK506 and its analogs – therapeutic potential for neurological disorders: A. Klettner and T. Herdegen; Curr. Drug Targets CNS Neurol. Disord. 2, 153 (2003), Review, Abstract
- FK506, an immunosuppressant targeting calcineurin function: F.J. Dumont; Curr. Med. Chem. 7, 731 (2000), Abstract
- Immunosuppressant FK506 activates NF-kappaB through the proteasome-mediated degradation of IkappaBalpha. Requirement for Ikappabalpha n-terminal phosphorylation but not ubiquitination sites: Y. Zhang, et al.; J. Biol. Chem. 274, 34657 (1999), Abstract — Full Text
- Cyclosporin A, FK506 and rapamycin: more than just immunosuppression: J. Kunz and M.N. Hall; TIBS 18, 334 (1993), Abstract
- Cyclosporin A and FK506: molecular mechanisms of immunosuppression and probes for transplantation biology: B.E. Bierer, et al.; Curr. Opin. Immunol. 5, 763 (1993), Abstract
- FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics: T. Kino, et al.; J. Antibiot. (Tokyo) 40, 1249 (1987), Abstract
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